KR102377805B1 - 피리미딘 및 그의 변이체, 및 그의 용도 - Google Patents

피리미딘 및 그의 변이체, 및 그의 용도 Download PDF

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KR102377805B1
KR102377805B1 KR1020187029805A KR20187029805A KR102377805B1 KR 102377805 B1 KR102377805 B1 KR 102377805B1 KR 1020187029805 A KR1020187029805 A KR 1020187029805A KR 20187029805 A KR20187029805 A KR 20187029805A KR 102377805 B1 KR102377805 B1 KR 102377805B1
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South Korea
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compound
mmol
mixture
formula
added
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KR1020187029805A
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KR20180128015A (ko
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로널드 찰스 홀리
프라바 이브라힘
안토니 피. 포드
조엘 알. 게버
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애퍼런트 파마슈티컬스 인크.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50Three nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
KR1020187029805A 2016-03-25 2017-03-20 피리미딘 및 그의 변이체, 및 그의 용도 KR102377805B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662313334P 2016-03-25 2016-03-25
US62/313,334 2016-03-25
PCT/US2017/023126 WO2017165255A1 (en) 2016-03-25 2017-03-20 Pyrimidines and variants thereof, and uses therefor

Publications (2)

Publication Number Publication Date
KR20180128015A KR20180128015A (ko) 2018-11-30
KR102377805B1 true KR102377805B1 (ko) 2022-03-22

Family

ID=59900805

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020187029805A KR102377805B1 (ko) 2016-03-25 2017-03-20 피리미딘 및 그의 변이체, 및 그의 용도

Country Status (11)

Country Link
US (2) US10662162B2 (es)
EP (1) EP3433258B1 (es)
JP (1) JP6902045B2 (es)
KR (1) KR102377805B1 (es)
CN (1) CN108779119B (es)
AU (1) AU2017237929B2 (es)
CA (1) CA3018180C (es)
MA (1) MA44489A (es)
MX (1) MX2018011622A (es)
RU (1) RU2760733C2 (es)
WO (1) WO2017165255A1 (es)

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* Cited by examiner, † Cited by third party
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MA43821A (fr) 2016-03-14 2018-11-28 Afferent Pharmaceuticals Inc Pyrimidines et variantes de celles-ci, et leurs utilisations
CA3018180C (en) 2016-03-25 2024-02-20 Ronald Charles Hawley Pyrimidines and variants thereof, and uses therefor
DK3555048T3 (da) 2016-12-19 2021-10-11 Novartis Ag Nye picolinsyrederivater og deres anvendelse som mellemprodukter
WO2018118668A1 (en) * 2016-12-20 2018-06-28 Afferent Pharmaceuticals, Inc. Crystalline salts and polymorphs of a p2x3 antagonist
WO2019085916A1 (zh) * 2017-11-01 2019-05-09 北京泰德制药股份有限公司 P2x3和/或p2x2/3受体拮抗剂、包含其的药物组合物及其用途
CN107778255B (zh) * 2017-11-16 2019-10-25 山东大学 一种二芳基嘧啶类hiv-1逆转录酶抑制剂及其制备方法和应用
MX2021013347A (es) * 2019-04-30 2022-01-24 Beijing Tide Pharmaceutical Co Ltd Metodo para tratar el dolor asociado con endometriosis mediante el uso de un compuesto de diaminopirimidina.
EP3964505A4 (en) * 2019-04-30 2022-12-21 Beijing Tide Pharmaceutical Co., Ltd. SOLID FORM OF DIAMINOPYRIMIDINE COMPOUND OR A HYDRATE THEREOF, METHOD FOR PREPARING IT AND APPLICATION
EP3960179A4 (en) * 2019-04-30 2023-01-25 Beijing Tide Pharmaceutical Co., Ltd. METHOD OF TREATMENT OF COUGH USING A DIAMINOPYRIMIDINE COMPOUND
CN113924293B (zh) * 2019-06-06 2024-07-09 北京泰德制药股份有限公司 P2x3和/或p2x2/3受体拮抗剂、包含其的药物组合物及其用途

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US2953567A (en) * 1956-11-23 1960-09-20 Burroughs Wellcome Co 5-phenylmercaptopyrimidines and method
WO2000059893A1 (en) * 1999-04-06 2000-10-12 Krenitsky Pharmaceuticals Inc. Neurotrophic thio substituted pyrimidines
ATE326462T1 (de) * 2000-12-21 2006-06-15 Vertex Pharma Pyrazolverbindungen als protein-kinase- inhibitoren
EP1725540B1 (en) * 2004-03-05 2012-09-12 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 antagonists
CN101296907B (zh) * 2005-09-01 2013-03-27 弗·哈夫曼-拉罗切有限公司 作为p2x3和p2x2/3调节剂的二氨基嘧啶类
CA2620129C (en) * 2005-09-01 2014-12-23 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
ES2601178T3 (es) * 2005-09-01 2017-02-14 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores de P2X3 y P3X2/3
JP4850914B2 (ja) * 2005-09-01 2012-01-11 エフ.ホフマン−ラ ロシュ アーゲー P2x3およびp2x2/3モジュレーターとしてのジアミノピリミジン
JP5128603B2 (ja) * 2006-10-04 2013-01-23 エフ.ホフマン−ラ ロシュ アーゲー フェノキシジアミノピリミジン誘導体の合成方法
WO2008104472A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag 2, 4 -diaminopyrimidine derivatives and their use as p2x antagonists or as prodrugs thereof
WO2008104474A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Diaminopyrimidines
EP2203429A1 (en) * 2007-10-31 2010-07-07 Nissan Chemical Industries, Ltd. Pyridazinone derivatives and use thereof as p2x7 receptor inhibitors
GB2471713A (en) 2009-07-08 2011-01-12 Univ Greenwich 1,2,4-triazine derivatives and their use as sodium channel blockers
TWI637949B (zh) * 2013-06-14 2018-10-11 塩野義製藥股份有限公司 胺基三衍生物及含有其等之醫藥組合物
JP6546592B2 (ja) * 2013-08-23 2019-07-17 アファレント ファーマシューティカルズ インコーポレイテッド 急性、亜急性または慢性の咳を治療するためのジアミノピリミジンp2x3およびp2x2/3受容体モジュレーター
WO2016004358A1 (en) * 2014-07-03 2016-01-07 Afferent Pharmaceuticals, Inc. Methods and compositions for treating diseases and conditions
MA43821A (fr) * 2016-03-14 2018-11-28 Afferent Pharmaceuticals Inc Pyrimidines et variantes de celles-ci, et leurs utilisations
CA3018180C (en) 2016-03-25 2024-02-20 Ronald Charles Hawley Pyrimidines and variants thereof, and uses therefor

Also Published As

Publication number Publication date
US20190055202A1 (en) 2019-02-21
CN108779119B (zh) 2022-02-08
US11230532B2 (en) 2022-01-25
AU2017237929B2 (en) 2021-04-15
RU2760733C2 (ru) 2021-11-30
US10662162B2 (en) 2020-05-26
JP6902045B2 (ja) 2021-07-14
RU2018137032A3 (es) 2020-05-22
CA3018180A1 (en) 2017-09-28
JP2019510025A (ja) 2019-04-11
RU2018137032A (ru) 2020-04-27
US20200239421A1 (en) 2020-07-30
KR20180128015A (ko) 2018-11-30
CA3018180C (en) 2024-02-20
MX2018011622A (es) 2019-03-28
BR112018069105A2 (pt) 2019-01-29
EP3433258A1 (en) 2019-01-30
CN108779119A (zh) 2018-11-09
AU2017237929A1 (en) 2018-09-13
EP3433258B1 (en) 2023-07-19
EP3433258A4 (en) 2019-10-30
MA44489A (fr) 2019-01-30
WO2017165255A1 (en) 2017-09-28

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